CVS drugs and pharmacology Flashcards
What receptors do epinephrine and norepinephrine act on?
Epinephrine: a and B adrenoreceptors.
Norepinephrine: a1 and 2, B1 adrenoreceptors
Action of epinephrine at B1 and B2 adrenoreceptors?
B1: Vasoconstriction and cardiac stimulant. Raises Systolic BP.
B2: Vasodilation at skeletal muscle blood vessels.
Action of norepinephrine at receptors?
Increases peripheral resistance and systolic/diastolic bp.
MOA and use of phenylephrine?
Is a selective a-1 adrenoreceptor agonist.
Causes vasoconstriction and raises bp.
Is used as a nasal decongestant, pupil dilator and vasopressor (e.g in postural hypotension).
i) MOA. and use of salbutamol?
ii) SE of salbutamol?
B adrenoreceptor agonist.
Causes vasodilation and drop in BP and relaxes smooth muscle.
Used inhaled to treat asthma (bronchodilation due to relaxation of airway smooth muscle).
SE= Arrythmias, Tachycardia, Headache
i) MOA and use of Phenoxybenzamine?
ii) SE’s of selective a-1 adrenoreceptors?
an adrenoreceptor antagonist. Blocks norepinephrine binding and prevents it’s reuptake.
Causes vasodilation and drop in BP and PR.
SE: Postural hypotension and impotence.
MOA and uses of Propranolol and Atenolol?
Propranolol: B blocker.
Atenolol: B blocker (B1, cardioselective)
- Treat cardiac arrhythmias, angina, MI, anxiety.
- SE: Bronchoconstriction, bradycardia, HF, cold extremities, insomnia, depression.
Features of Nicotinic receptors?
- Ach binds, influx of Na+ and efflux of K+, prop of AP, Ca2+ release, activation of contractile machinery.
- Ligand-gated ion channels
- Fast excitary transmission
- Nm and Nn types
Features of Muscarinic receptors?
- M1, M2, M3 types.
- M1 and 3 acts via IP pathway (prod. IP3 and DAG)
- M2 inhibits adenylate cyclase (inhibit cAMP).
MOA and use of Pilocarpine?
Direct muscarinic agonist.
Increases sec. by exocrine glands.
Binds to M3 rec, prod. IP3 and DAG, Ca2+ release, binds to caldesmon, actin-myosin interactions, muscle contracts.
Can be used to treat glaucoma (drains aqueous humour)
MOA. and use of Nicotine?
Direct nicotinic agonist.
Binds to both Nm and Nn.
Can be used in smoking cessation.
Causes vasoconstriction and increases bp.
MOA, uses and examples of Anti-acetylcholinesterases?
Bind to AchE, prevent hydrolysis of Ach, therefore increase the effects of Ach.
- Short acting (Edrophonium)
- Used to diagnose MG.
- Medium acting (Neostigmine, Physostigmine)
- Treats glaucoma.
- Irreversible (Sarin)
- Insecticides, war gases
Consequences of Anti-AchE poisoning?
Antidotes to Anti-AchE poisoning?
SLUDGE Syndrome Bradycardia Hypotension Hypersecretion Bronchoconstriction GIT hypermotility Increased intraocular pressure.
Antidote?
- Atropine
- Oxime
MOA and use of Atropine?
Cholinergic receptor antagonist.(comp)
Causes pupil dilation, inhibits secretions.
SE: Restlessness, agitation, disorientation, body temp increase.
MOA of Nitrates in treating Angina and other uses?
Nitrate=> NO=> Activates guanylyl cyclase=> prod. cGMP=> Activates protein kinases=> Phosp. myosin light chains=> Decreases ic Ca2+=> Vascular relaxation.
Route?
- Orally
- Sublingually
- Cutaneously
- IV
Treats?
- SA, UA, MI, HF, Hypertension
SE’s?
- Headache, hypotension (especially with phosphodiesterase 5 inhibitors)